Synergized hypnotic and sedative



. 1,716,686, granted July 11 Patented Nov. 3,1931

UNITED STATES PATENT. ounce MOSES L CBOSSLEY, OF PLAINFIELD, NEW JERSEY, ASSIGNOR, BY KESNE ASSIGN- MIENTS, TO THE GALCO CHEMICAL COMPANY, INC A CORPORATION 01' DELAWARE mmmmb mrnrorrc m smwnvn R Drawing.

My invention relates particularly to improved pharmaceuticals having enhanced economic value and ,more extended use in chemotherapyfbut especiall it has relation to improvedhypnotics an sedatives containing one or more magnesium compounds which synergize the drugs present.

In my co-pending application, Serial No. 178,152, filed March 24,1927, Patent Number 1929, I have disclosed pharmaceuticals having enhanced therapeutic value owing to the synergizing of the drugs therein, having" known therapeutic properties, with magnesium compounds. As set forth therein, the therapeutic range of the drugs is increased by their otentiation due to the magnesium compoun s present. That is to say, a 'ven therapeutic effect can be attained, accor ing- 0 ly, with less of the potentiated dru than when unpotentiated, and with less anger to the patient from an toxic action on the human organism.- As have shown therein, furthermore, the potenti'ated drugs have a distinct economic advantage as compared with the unpotentiated drugs. Likewise, there is less tendency, when using the same, to cause secondary efiects than in the case of the unpotentiated drug, and, accordingly, the human system is better able to toleratethe drugs. I find, furthermore, that the drugs are also 1e s liable to accumulate in'the sys' tem inasmuch as the desired therapeutic effect can be obtained with smaller egoses;-which' 1 5 is a very decided advantage,

pecially in the case of haEit-forming drugs.

The object f my invention is to provide improved pharmaceuticals, and particularly those used because of their hypnotic and se-;i dative properties, inwhich the drugs have.

their therapeutic properties potentiated due to the presence of one or more magnesiumcompounds. f-The object of my invention is; more particularly, furthermore, to

4 provide a composition of this character a lication fled April 17, ms. Serial Io. 270,808.-

containin a drug of thelbarbituric acid series, the ormula for barbituricacid being which, by reason ofthe presence of a magnesium compound will produce their own therapeutic eflects with much less of the drug and in a shorter time than in the case of the unpotentiated drug. It is found, furthermore, that in using the composition made in accordance with my invention, the narcosis which results from the drug is less prolonged than with the unpotentiated drug. Also, the composition is less toxic in therapeutic doses than with the unpotentiated drug. With these com ositions containing hypnotic and sedative rugs, such, for example, as the drugs of the barbituric acid series,oneexample of which is bartital or some other hypnotic and-sedative such as bromatone, bromural, carbromal, chloral, sulfonal, etc., and containing one or more magnesium compounds as above referred to, such, for example, as

-magnesium chloride, magnesium sulfate,

magnesium oxide, magnesium lactate, margnesium gluconate, etc.,I may use other ad tionaL compositions which may or may not have a therapeutic effect. Such substances which may be added to enhance the absorptive properties of the composition are, for example, ethyl alcohol, glycerol, glycol, etc. Also, in all such compositions the magnesium compound ma vary in amount through wide limits, but I ave found very effective results .to be obtained by the use of the magnesium compound in an amount in which the magnesium present is at least 25% by weight of the, weight of the drug present.

My invention is capable of being carried out in many difierent ways but for the pur- I pose of illustration I shall describe onlycertain forms of carrying out the same in detail hereinafter. I i

For example, an effective composition made in accordance with my invention may contain 2 parts by weight of magnesium chloride and 1 part *by' weight of sodium barbital,

the formula of which isonset of the narcosis accelerated when using p said composition, but it is found that the animal recovers much more quickly as the narcosis is less prolonged. In many cases I have found that thenarcotic condition produced by the synergic combination is over in about one half the time required for the recovery by using the unpotentiated dose required to produce a similar degree of narcosis. Barbital alone is usually administered in 5 grain tablets. I have found that, instead, a tablet containing approximately 2 grains of-barbital and 5 grains of magnesium chloride or an equivalent weight of magnesium oxide, can be used with the same therapeutic effects. It will be understood that the proportion of the'magnesium compound used may be widely varied and may, for exam le, be increased to as large a quantity as found efiective for the purpose desired, or substituted by any other Imagnesium compound as above described. t will also be understood that any other one of the hypnotic and sedative drugs may be substituted for the barbital, if desired. Also, while 4 the composition above described, as well as those hereinafter referred to, or their components, may be administered per os, they may be administered in any other way, as, for

example, by injection (intravenously or intramuscularly) or by any suitable method, employed in medicine.

Again, it will be understood the synergic compositions may be made of the above character, but containing, also, some substance to increase the absorption, as, for example, aloohol, glycerine or glycol or some other suitable polyhydroxyl alcohol. A compositionof this character may be comprised of 0.2 parts by weight of sodium barbital, 0.4 parts by weight of magnesium' cbloride, and 30 parts by weight of- 2 2%" alcohol. If desired, there maybe added, also, 10'parts by weight of a sweetening agent, such as sucrose syrup.

this composition it will 'be understoodflof course, that any other hypnotic and sedative drug .may be substituted for the sodium barbital. Also, any other one of the above mentioned magnesium compounds may be substituted in an equivalent quantity for the magnesium chloride, and thatthe quantity of the magnesium compound may be varied. in the manner referred to in the above mentioned compositions. Also, the alcohol may be substituted by any other one of the substances'hereinabove referred to for increasing the absorption of the composition. In fact any of the above constituents may be substituted by others of a similar character for similar purposes.

It will be understood, of course, that in all of the above compositions theproportions of the various constituents may be varied widely without departing from the spirit of my invention.

Synergic compositions of the above character are particularly effective in. the case of insomnia .and similar maladies.

While I have described my invention above in detail I wish'it to be understood that many changes may be made therein without depart ing from the spirit of the same.

.I claim: 1. A pharmaceutical product comprising a synergic composition containing a magnesium compound and a synthetic hypnotic and sedative drug, the them utic properties of which are increased by t e magnesium com-- pound.

2. A pharmaceuticalproduct comprising a synergic composition containing a magnesium compound and a drug of the barbituric acid group, the therapeutic properties of which are lncreased pound.

3. A pharmaceutical product comprising a synergic composition containing a magneslum compound and barbital, the therapeutic properties of which are creased by the magnesium compound. 4. A harmaceutical product-comprising a ergic composition containing magnesium by the magnesium comc oride, a synthetic hypnotic and'sedative" drug, the therapeutic properties of which are increased b the magnesium chloride, and an aliphatic a cohol, Y

- 5. Apharmaceutical product comprisinga synerg c compositioncontainin magnesium chloride, a drug of the barbitune acid group,

the therapeutic properties of which are m-- creased by the magnesium chloride, and an aliphatic alcohol.

6. A pharmadeutical product comprising}; synergic. composition containin magnesium c loride,barbital, the therapeutic PFP of which are mcreasedby chloride, and an aliphatic alcohol.

. 7. A pharmaceutical product comprising a synergiccompos'ition containing a magne ,the magnesium sium com ound and a synthetic hypnotic and sedativeug, the-thera eufic properties of which are increased by the magnesium com- I pound,the magnesium compound bein pres- 5 cut in an al'nout such that the-magneslum is at least 25% by weight of the drug present. 8. A pharmaceutical product comprising a er ic composition containin a magnei li m ompound and a'drug of this barbituric acid group, the therapeutic properties of which are increased by the magnesium com pound; the magnesium compound being present in an amout such that the magneslum is at least 25% by weight of the drug present.

9'. A pharmaceutical product comprising a 'synergic composition containing a magnesium com-pound and barbita'l, the therapeutic properties of which are increased by themagneslum compound, the magnesium compound being present in an amout such'that the magnesium is at least 25% by weight of the drug present.

In testimony that I claim the foregoing, I have hereunto set' my hand this 12th day of 26 April, 1928. a v a 'MOSES L. GROSSLEY. 

